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Synthesis of 2‑Arylindoles by Rhodium-Catalyzed/Copper-Mediated Annulative Coupling of N‑Aryl-2-aminopyridines and Propargyl Alcohols via Selective C–H/C–C Activation

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journal contribution
posted on 08.09.2019, 16:03 by Xufei Yan, Runyou Ye, Huihui Sun, Jing Zhong, Haifeng Xiang, Xiangge Zhou
A versatile rhodium-catalyzed/copper-mediated C–H/C–C activation and cascade annulation reaction was described to form 2-arylindole derivatives. Highly selective C–C bond cleavage of γ-substituted tert-propargyl alcohols occurred, together with pyridine-directed ortho C­(sp2)–H bond activation, affording a series of 2-arylindoles with yields up to 90%. Subsequent derivations were smoothly conducted to access polyfunctionalized 2-arylindoles, illustrating the potential applications of this method.